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61. 发明申请

US20120264765A1 Cyclohexane-1,3-Diones for Use in the Treatment of Amyotrophic Lateral Sclerosis 有权
标题翻译：用于治疗肌萎缩性侧索硬化症的环己烷-1,3-二酮
公开(公告)号：US20120264765A1
公开(公告)日：2012-10-18
申请号：US13504893
申请日：2010-10-29
申请人： Donald R. Kirsch , Radhia Benmohamed , Anthony C. Arvanties , Richard I. Morimoto , Wei Zhang , Richard B. Silverman
发明人： Donald R. Kirsch , Radhia Benmohamed , Anthony C. Arvanties , Richard I. Morimoto , Wei Zhang , Richard B. Silverman
IPC分类号： A61K31/122 , C07C49/697 , C07C49/753 , C07C225/22 , C07D295/205 , A61P25/28 , C07D307/46 , A61K31/136 , A61K31/495 , A61K31/403 , A61K31/341 , C07C49/657 , C07D209/86
CPC分类号： C07C69/75 , A61K31/136 , C07C49/563 , C07C49/567 , C07C49/577
摘要： The present invention relates to the identification of provided cyclohexane-1,3-diones (CHD compounds) and pharmaceutical compositions thereof for treating subjects with amyotrophic lateral sclerosis (ALS) and other neurodegenerative diseases. The invention also provides methods of preparing the provided CHD compounds.
摘要翻译：本发明涉及提供的环己烷-1,3-二酮（CHD化合物）及其药物组合物的鉴定，用于治疗肌萎缩性侧索硬化（ALS）和其它神经变性疾病的受试者。本发明还提供了制备所提供的CHD化合物的方法。

62. 发明申请

US20100222426A1 Anti-Bacterial Agents 审中-公开
标题翻译：抗菌剂
公开(公告)号：US20100222426A1
公开(公告)日：2010-09-02
申请号：US12677912
申请日：2008-09-15
申请人： Simon Gibbons , John P. Malkinson , Winnie Shiu
发明人： Simon Gibbons , John P. Malkinson , Winnie Shiu
IPC分类号： A61K31/335 , C07C49/657 , C07D303/34 , A61K31/12 , A61P31/04
CPC分类号： C07C49/84 , C07C45/46 , C07C45/673 , C07C45/78 , C07C49/825
摘要： The invention relates to novel acylphloroglucinols which have strong growth inhibitory effects on multi-drug resistant strains of bacteria, particularly MRSA. Typically the compounds have a terpene substituent, or a terpene-derived substituent. Methods of isolating the compounds from natural sources, and synthetic methods for forming the compounds are also provided.
摘要翻译：本发明涉及对细菌，特别是MRSA的多药耐药菌株具有强烈的生长抑制作用的新型酰基间苯三酚。通常，化合物具有萜烯取代基或来自萜烯的取代基。还提供了从天然来源分离化合物的方法，以及用于形成化合物的合成方法。

63. 发明授权

US5684205A Use of substituted cyclopentane- di- and -triones 失效
标题翻译：使用取代的环戊烷二 - 和二
公开(公告)号：US5684205A
公开(公告)日：1997-11-04
申请号：US525871
申请日：1995-09-08
申请人： Peter Norman , Roderick L. Hall , Graham A. Place , Graham Holmwood , Gabriele Braunlich
发明人： Peter Norman , Roderick L. Hall , Graham A. Place , Graham Holmwood , Gabriele Braunlich
IPC分类号： C07D333/22 , A61K31/12 , A61K31/135 , A61K31/38 , A61K31/381 , A61K31/44 , A61K31/4418 , A61P1/00 , A61P1/12 , A61P9/10 , A61P11/00 , A61P11/08 , A61P29/00 , C07C13/28 , C07C25/18 , C07C39/17 , C07C39/23 , C07C43/21 , C07C43/23 , C07C49/657 , C07C49/683 , C07C49/693 , C07C49/697 , C07C49/747 , C07C49/753 , C07C69/712 , C07C69/738 , C07C69/96 , C07C205/45 , C07C211/45 , C07C211/50 , C07C211/52 , C07C225/22 , C07D213/50 , C07C45/45
CPC分类号： C07C205/45 , C07C225/22 , C07C49/657 , C07C49/683 , C07C49/697 , C07C49/747 , C07C49/753 , C07C69/738 , C07C2101/08 , C07C2101/10
摘要： The invention relates to the use of substituted cyclopentane-diones and cyclopentane-triones for the preparation of medicaments which as chloride channel blockers are suitable for controlling airway diseases, secretory diarrhea and inflammatory diseases.
摘要翻译：本发明涉及取代的环戊烷二酮和环戊烷二硫代磷酸酯用于制备药物的用途，其作为氯化物通道阻断剂适合于控制气道疾病，分泌性腹泻和炎性疾病。

64. 发明授权

US5571831A Imidazole derivative, and pharmaceutical composition 失效
标题翻译：咪唑衍生物和药物组合物
公开(公告)号：US5571831A
公开(公告)日：1996-11-05
申请号：US486141
申请日：1995-06-07
申请人： Koichi Niimura , Takao Ando , Toyohiko Nitta , Yuko Ikeda
发明人： Koichi Niimura , Takao Ando , Toyohiko Nitta , Yuko Ikeda
IPC分类号： C07C45/62 , C07C45/68 , C07C49/657 , C07C49/683 , C07C49/697 , C07C49/747 , C07C255/56 , C07D233/60 , C07D249/08 , C07D303/04 , C07D303/08 , C07D303/14 , C07D303/46 , C07D521/00 , A61K31/415
CPC分类号： C07D231/12 , C07C255/56 , C07C45/62 , C07C45/68 , C07C49/657 , C07C49/683 , C07C49/697 , C07C49/747 , C07D233/56 , C07D249/08 , C07D303/04 , C07D303/08 , C07D303/14 , C07D303/46 , C07C2101/14 , C07C2101/16
摘要： A novel imidazole derivative of the formula (I): ##STR1## wherein X.sub.1 is a chlorine or fluorine atom, or a hydroxy group or a salt thereof, and a pharmaceutical composition containing the same as the active ingredient.
摘要翻译：式（I）的新型咪唑衍生物：其中X1为氯或氟原子，或羟基或其盐，和含有该活性成分的药物组合物。

65. 发明授权

US5547973A Method of inhibiting aromatase 失效
标题翻译：抑制芳香酶的方法
公开(公告)号：US5547973A
公开(公告)日：1996-08-20
申请号：US486142
申请日：1995-06-07
申请人： Koichi Niimura , Takao Ando , Toyohiko Nitta , Yuko Ikeda
发明人： Koichi Niimura , Takao Ando , Toyohiko Nitta , Yuko Ikeda
IPC分类号： C07C45/62 , C07C45/68 , C07C49/657 , C07C49/683 , C07C49/697 , C07C49/747 , C07C255/56 , C07D233/60 , C07D303/04 , C07D303/08 , C07D303/14 , C07D303/46 , C07D521/00 , A61K31/415
CPC分类号： C07D231/12 , C07C255/56 , C07C45/62 , C07C45/68 , C07C49/657 , C07C49/683 , C07C49/697 , C07C49/747 , C07D233/56 , C07D249/08 , C07D303/04 , C07D303/08 , C07D303/14 , C07D303/46 , C07C2101/14 , C07C2101/16
摘要： A method of inhibiting aromatase, comprising administering to a mammal in need thereof a pharmaceutical composition comprising an effective aromatase inhibiting amount of a compound of the formula (I): ##STR1## wherein X.sub.1 is a chlorine or fluorine atom, or a hydroxy group, or a pharmaceutically acceptable salt thereof, and a pharmaceutically acceptable carrier.
摘要翻译：一种抑制芳香酶的方法，其包括向有需要的哺乳动物施用包含有效芳香酶抑制量的式（I）化合物的药物组合物：其中X 1是氯或氟原子，或羟基或其药学上可接受的盐和药学上可接受的载体。

66. 发明授权

US5403953A 1-phenylbicyclo[2.2.2]octane compounds 失效
标题翻译： 1-苯基双环[2.2.2]辛烷化合物
公开(公告)号：US5403953A
公开(公告)日：1995-04-04
申请号：US156299
申请日：1993-11-23
申请人： Guillaume de Nanteuil , Michel Vincent , Christine Lila , Jacqueline Bonnet , Armel Fradin
发明人： Guillaume de Nanteuil , Michel Vincent , Christine Lila , Jacqueline Bonnet , Armel Fradin
IPC分类号： A61K31/13 , A61K31/16 , A61K31/19 , A61K31/235 , A61K31/275 , A61K31/47 , A61P29/00 , C07C17/16 , C07C23/32 , C07C43/196 , C07C45/45 , C07C45/56 , C07C45/59 , C07C45/71 , C07C47/575 , C07C49/657 , C07C49/753 , C07C49/84 , C07C57/46 , C07C59/54 , C07C59/72 , C07C62/34 , C07C65/26 , C07C69/708 , C07C69/757 , C07C229/14 , C07C229/38 , C07C229/48 , C07C233/58 , C07C235/06 , C07C235/40 , C07C235/42 , C07C237/24 , C07C255/47 , C07C321/22 , C07C323/52 , C07D215/48 , C07D215/50 , C07D307/24 , C07D307/30 , C07D307/80 , C07D307/84 , C07D309/08 , C07D309/28 , C07D311/76 , C07C62/06
CPC分类号： C07D307/80 , C07C17/16 , C07C23/32 , C07C235/06 , C07C235/42 , C07C323/52 , C07C43/196 , C07C45/45 , C07C45/565 , C07C45/59 , C07C45/71 , C07C47/575 , C07C49/657 , C07C49/753 , C07C49/84 , C07C59/54 , C07C59/72 , C07C65/26 , C07C69/708 , C07D215/50 , C07C2102/44
摘要： Compound of formula (I): ##STR1## in which: R.sub.1 represents halogen, or hydroxy, alkyl, alkoxy, cyano, amino, mercapto, alkylthio or phenoxy,R.sub.2 and R'.sub.2 represent two hydrogen when the ring is unsaturated, or alternatively identical or different, represent hydrogen or halogen, or hydroxy, alkyl, alkoxy, cyano, amino or oxo when the ring is saturated,R.sub.3 represents any one of the following groups: ##STR2## in which: m represents 1, 2 or 3,X represents oxygen or sulfur or N-R, R.sub.5 or R.sub.6, which are identical or different, represent hydrogen or alkyl or trifluoromethyl or form (C.sub.3 -C.sub.6) cycloalkyl,n represents 0, 1 or 2,R.sub.7 represents hydroxy, alkoxy, amino, or --O--CH.sub.2 --CO--NRR',R.sub.4 represents hydrogen or halogen or alkyl, alkoxy or trihaloalkyl.
摘要翻译：式（I）化合物：其中：R 1表示卤素，或羟基，烷基，烷氧基，氰基，氨基，巯基，烷硫基或苯氧基，当环为不饱和时，R 2和R'2表示两个氢或者相同或不同，当环饱和时，R 3表示氢或氢，羟基，烷基，烷氧基，氰基，氨基或氧代，R 3表示以下基团中的任何一个：CO 2 H CONHCH 2 CO 2 H（CH 2）m CO 2 H

67. 发明授权

US5248830A Enantioselective preparation of acetylenic or olefinic substituted cycloalkenyl dihydroxybutyrates and 4-hydroxy-tetrahydro-pyran-2-ones 失效
标题翻译：炔属或烯烃取代的环烯基二羟基丁酸酯和4-羟基 - 四氢 - 吡喃-2-酮的对映选择性制备
公开(公告)号：US5248830A
公开(公告)日：1993-09-28
申请号：US902752
申请日：1992-06-23
申请人： John Ullrich , John R. Regan
发明人： John Ullrich , John R. Regan
IPC分类号： C07C45/58 , C07C49/657 , C07C49/697 , C07C49/747 , C07C49/753 , C07C69/732 , C07C69/738 , C07C205/45 , C07F7/08 , C07F7/18 , C07F9/30 , C07F9/32
CPC分类号： C07F9/3223 , C07C205/45 , C07C45/58 , C07C49/657 , C07C49/697 , C07C49/747 , C07C49/753 , C07C69/732 , C07C69/738 , C07F7/0818 , C07F7/186 , C07F9/303
摘要： Disclosed are intermediates and a process of making an anticholesterolemic compound of the formula ##STR1## the corresponding ring-opened hydroxy acids derived therefrom and pharmaceutically acceptable salts thereof.
摘要翻译：公开了中间体和制备下式的抗胆固醇血型化合物的方法：由其衍生的相应的开环羟基酸及其药学上可接受的盐。

68. 发明授权

US5159118A Cyclopentanone derivatives 失效
标题翻译：环戊酮衍生物
公开(公告)号：US5159118A
公开(公告)日：1992-10-27
申请号：US691406
申请日：1991-04-25
申请人： Satoru Kumazawa , Susumu Shimizu , Hiroyuki Enari , Atsushi Ito , Susumu Ikeda , Nobuo Sato , Toshihide Saishoji
发明人： Satoru Kumazawa , Susumu Shimizu , Hiroyuki Enari , Atsushi Ito , Susumu Ikeda , Nobuo Sato , Toshihide Saishoji
IPC分类号： A01N43/50 , A01N43/653 , C07C1/00 , C07C13/28 , C07C17/00 , C07C17/26 , C07C25/18 , C07C45/00 , C07C45/67 , C07C49/657 , C07C49/697 , C07C67/00 , C07C69/716 , C07D233/60 , C07D249/08 , C07D303/04 , C07D303/08 , C07D521/00
CPC分类号： C07D231/12 , A01N43/50 , A01N43/653 , C07C13/28 , C07C25/18 , C07C45/676 , C07C49/657 , C07C49/697 , C07D233/56 , C07D249/08 , C07D303/04 , C07D303/08
摘要： Disclosed herein are an azole derivative represented by the formula(I): ##STR1## wherein R.sup.1 and R.sup.2 respectively represent a (C.sub.1 -C.sub.5) alkyl group or a hydrogen atom; X represents a halogen atom, a (C.sub.1 -C.sub.5) alkyl group or a phenyl group; n represents an integer of from 0 to 2 and A represents a nitrogen atom or a CH, provided that R.sup.1 is not a hydrogen atom when R.sup.2 is a hydrogen atom, a process for producing the azole derivative represented by the formula(I), and an agricultural and horticultural composition containing the azole derivative represented by the formula(I).
摘要翻译：本文公开的是由式（I）表示的唑衍生物：其中R 1和R 2分别表示（C 1 -C 5）烷基或氢原子; X表示卤素原子，（C1-C5）烷基或苯基; n表示0〜2的整数，A表示氮原子或CH，条件是当R 2为氢原子时，R 1不为氢原子，由式（I）表示的唑衍生物的制造方法，以及含有由式（I）表示的唑衍生物的农业和园艺组合物。

69. 发明授权

US5110989A Herbicidal compounds and compositions 失效
标题翻译：除草剂及组合物
公开(公告)号：US5110989A
公开(公告)日：1992-05-05
申请号：US553413
申请日：1990-07-17
申请人： Alexander Serban , Keith G. Watson , Graham J. Bird , Graeme J. Farquharson , Linsay E. Cross
发明人： Alexander Serban , Keith G. Watson , Graham J. Bird , Graeme J. Farquharson , Linsay E. Cross
IPC分类号： C07C1/22 , C07C17/00 , C07C45/45 , C07C45/46 , C07C45/65 , C07C45/67 , C07C45/74 , C07C47/546 , C07C47/55 , C07C47/575 , C07C49/657 , C07C49/697 , C07C49/747 , C07C49/753 , C07C49/835
CPC分类号： C07C1/22 , C07C17/35 , C07C45/455 , C07C45/46 , C07C45/65 , C07C45/673 , C07C45/74 , C07C47/546 , C07C47/55 , C07C47/575 , C07C49/657 , C07C49/697 , C07C49/747 , C07C49/753 , C07C49/835 , C07C2102/08
摘要： The invention concerns novel compounds of the formula I ##STR1## wherein: W are selected from alkyl, alkenyl and alkynyl;X are selected from halogen, nitro, cyano, alkyl, substituted alkyl, hydroxy, alkoxy, substituted alkoxy, alkenyl, alkynyl, alkenyloxy, alkynyloxy, acyloxy, alkoxycarbonyl, alkylthio, alkylsulfinyl, alkylsulfonyl, sulfamoyl, substituted sulfamoyl, amino, substituted amino, and the groups formyl and alkanoyl and the oxime, imine and Schiff base derivatives thereof, and an alkylene group which bridges two adjacent carbon atoms of the benzene ring;R.sup.1 is selected from hydrogen, alkyl, alkenyl, alkynyl, substituted alkyl, alkylsulfonyl, arylsulfonyl, acyl and an inorganic or organic cation;R.sup.2 is selected from alkyl, substituted alkyl, alkenyl, haloalkenyl, alkynyl and haloalkynyl;R.sup.3 is selected from alkyl, fluoroalkyl, alkenyl, alkynyl, and phenyl;p is zero or an integer selected from 1 to 4;n is zero or an integer selected from 1 to 3; andm is zero or an integer selected from 1 to 3.The compounds of the invention show cereal selective herbicidal properties and plant growth regulating properties and in further embodiments the invention provides processes for the preparation of the compounds of formula I, intermediates useful in the preparation of the compounds of formula I, compositions containing as active ingredient a compound of formula I, and herbicidal and plant growth regulating processes utilizing compounds of formula I.
摘要翻译：本发明涉及式I的新型化合物其中：W选自烷基，烯基和炔基; X选自卤素，硝基，氰基，烷基，取代的烷基，羟基，烷氧基，取代的烷氧基，烯基，炔基，烯氧基，炔氧基，酰氧基，烷氧基羰基，烷硫基，烷基亚磺酰基，烷基磺酰基，氨磺酰基，取代氨磺酰基，氨基，取代的氨基，和甲酰基和烷酰基以及其肟，亚胺和席夫碱衍生物和桥接苯环的两个相邻碳原子的亚烷基; R 1选自氢，烷基，烯基，炔基，取代的烷基，烷基磺酰基，芳基磺酰基，酰基和无机或有机阳离子; R2选自烷基，取代的烷基，烯基，卤代烯基，炔基和卤代炔基; R3选自烷基，氟烷基，烯基，炔基和苯基; p为零或选自1至4的整数; n为0或选自1至3的整数; 本发明的化合物显示谷物选择性除草性质和植物生长调节性质，并且在进一步的实施方案中，本发明提供了制备式I化合物的方法，可用于式I化合物的制备，含有式I化合物作为活性成分的组合物，以及利用式I化合物的除草和植物生长调节方法。

70. 发明授权

US5000961A Tert-butyl derivatives of benzylidenecamphor, process for preparing them, their use as antioxidant agents and cosmetic and pharmaceutical compositions containing them 失效
标题翻译：亚苄基樟脑的叔丁基衍生物，其制备方法，它们作为抗氧化剂的用途和含有它们的化妆品和药物组合物
公开(公告)号：US5000961A
公开(公告)日：1991-03-19
申请号：US528013
申请日：1990-05-23
申请人： Gerard Lang , Serge Forestier , Alain Lagrange , Claudine Moire , Andre Deflandre
发明人： Gerard Lang , Serge Forestier , Alain Lagrange , Claudine Moire , Andre Deflandre
IPC分类号： C07C49/683 , A21D2/14 , A61K8/00 , A61K8/04 , A61K8/11 , A61K8/30 , A61K8/34 , A61K8/92 , A61K9/00 , A61K31/12 , A61K31/125 , A61Q1/00 , A61Q5/02 , A61Q5/04 , A61Q5/08 , A61Q5/10 , A61Q17/04 , A61Q19/00 , C07C45/00 , C07C45/45 , C07C45/72 , C07C45/74 , C07C49/657 , C07C49/743 , C07C49/747 , C07C49/753 , C07C67/00 , C09K3/00 , C09K15/06 , C09K15/08
CPC分类号： A61Q17/04 , A61K8/35 , C07C45/74 , C07C49/747 , C07C49/753 , Y10S514/88 , Y10S514/886 , Y10S514/937
摘要： The invention relates to benzylidenecamphor derivatives of formula: ##STR1## where R is hydrogen or a tert-butyl residue, R.sub.1 is a C.sub.1 -C.sub.8 alkyl or alkoxy residue, and R.sub.2 and R.sub.3 denote hydrogen or hydroxyl, at least one of the two being hydroxyl, to a process for preparing them and to their uses as antioxidants, broad-band sunscreens and medicinal products for the preventive treatment of skin allergies and inflammations as well as for the prevention of certain cancers.

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